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54

Inhibitors & Agonists

1

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Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12704
    ITD-1
    5 Publications Verification

    		 TGF-β Receptor Cardiovascular Disease
    ITD-1 is the first selective TGFβ receptor inhibitor with an IC50 of 460 nM.
    ITD-1
  • HY-137063
    (+)-ITD-1

    		TGF-beta/Smad TGF-β Receptor Cardiovascular Disease
    (+)-ITD-1 is an inhibitor for TGF-β, that inhibits the TGF-β2 with an IC50 of 0.46 μM. (+)-ITD-1 promotes the degradation of TGF-b type II receptor (TGFBR2) and the differentiation of cardiomyocyte, and inhibits the mesoderm formation in the early differentiation stage of mouse embryonic stem cells (mESCs) .
    (+)-ITD-1
  • HY-144709
    FLT3/ITD-IN-1

    		FLT3 Cancer
    FLT3/ITD-IN-1 (Compound 1) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 38.2 nM and 144.1 nM against FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-1 displays excellent antiproliferative activities against acute myeloid leukemia cell lines .
    FLT3/ITD-IN-1
  • HY-160848
    FLT3/ITD-IN-5

    		FLT3 Cancer
    FLT3/ITD-IN-5 (Example 6) is an orally active FLT3 and FLT3-ITD inhibitor, with IC50 values of 0.088 and 0.348 nM, respectively. FLT3/ITD-IN-5 can be used for the research of cancer .
    FLT3/ITD-IN-5
  • HY-144710
    FLT3/ITD-IN-2

    		FLT3 Cancer
    FLT3/ITD-IN-2 (Compound 17) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 0.3, 0.4 and 1.0 nM against FLT3 D835Y, FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-2 potently inhibits the phosphorylation of FLT3 and displays excellent antiproliferative activities against acute myeloid leukemia cell lines .
    FLT3/ITD-IN-2
  • HY-144711
    FLT3/ITD-IN-3

    		FLT3 Cancer
    FLT3/ITD-IN-3 (Compound 19) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 0.3, 0.4 and 0.9 nM against FLT3 D835Y, FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-3 potently inhibits the phosphorylation of FLT3 and displays excellent antiproliferative activities against acute myeloid leukemia cell lines .
    FLT3/ITD-IN-3
  • HY-146680
    FLT3/ITD-IN-4

    		FLT3 RET CDK MAP4K Cancer
    FLT3/ITD-IN-4 (Compound 16) is a selective FMS-like tyrosine kinase 3 internal tandem duplications (FLT3-ITD) inhibitor with an IC50 of 2.3 nM. FLT3/ITD-IN-4 can be used for acute myeloid leukemia research .
    FLT3/ITD-IN-4
  • HY-168741
    FLT3-ITD-IN-2

    		FLT3 Cancer
    FLT3-ITD-IN-2 (Compound A1) is an inhibitor for FLT3-ITD kinase with an IC50 of 2.12 nM. FLT3-ITD-IN-2 inhibits the proliferation of FLT3-dependent human AML cell line MOLM-13 with an IC50 of 25.65 nM. FLT3-ITD-IN-2 exhibits antitumor efficacy against acute myeloid leukemia .
    FLT3-ITD-IN-2
  • HY-123201
    KRN383 analog

    		FLT3 Cancer
    KRN383 analog is an analog of KRN383. KRN383 is an orally active Flt3 inhibitor that inhibits the autophosphorylation of Flt3 bearing internal tandem duplications (ITDs) and the Asp835Tyr (D835Y) point mutation with IC50 values of < or =5.9 and 43 nM, respectively. KRN383 also inhibits the proliferation of the ITD-positive cell lines with IC50 values of < or =2.9 nM. KRN383 can be used for the research of acute myeloid leukemia .
    KRN383 analog
  • HY-161323
    FLT3-ITD/D835Y-IN-1

    		FLT3 Bcr-Abl Apoptosis Cancer
    FLT3-ITD/D835Y-IN-1 (Compound 1) is a FLT3-ITD and BCR-ABL inhibitor. FLT3-ITD/D835Y-IN-1 mediates proapoptosis by inhibiting the FLT3 and BCR-ABL pathways, as well as other possible targets. FLT3-ITD/D835Y-IN-1 can be used in the study of acute myeloid leukemia (AML) .
    FLT3-ITD/D835Y-IN-1
  • HY-145903
    PDGFRα/FLT3-ITD-IN-2

    		PDGFR FLT3 Cancer
    PDGFRα/FLT3-ITD-IN-2 (Compound 13d) is a potent inhibitor of PDGFRα/FLT3 with IC50s of more than 20 and 1.654 μM, respectively. PDGFRα/FLT3-ITD-IN-2 has the potential for the research of acute myeloid leukemia or chronic eosinophilic leukemia .
    PDGFRα/FLT3-ITD-IN-2
  • HY-145904
    PDGFRα/FLT3-ITD-IN-3

    		PDGFR FLT3 Cancer
    PDGFRα/FLT3-ITD-IN-3 (Compound 18d) is a potent inhibitor of PDGFRα/FLT3 with IC50s of 0.153 and 0.004 μM, respectively. PDGFRα/FLT3-ITD-IN-3 has the potential for the research of acute myeloid leukemia or chronic eosinophilic leukemia .
    PDGFRα/FLT3-ITD-IN-3
  • HY-145902
    PDGFRα/FLT3-ITD-IN-1

    		PDGFR FLT3 Cancer
    PDGFRα/FLT3-ITD-IN-1 (Compound 12d) is a potent inhibitor of PDGFRα/FLT3 with IC50s of more than 0.036 and 0.003 μM, respectively. PDGFRα/FLT3-ITD-IN-1 has the potential for the research of acute myeloid leukemia or chronic eosinophilic leukemia .
    PDGFRα/FLT3-ITD-IN-1
  • HY-145691
    HP1142

    		FLT3 Cancer
    HP1142 is a potent and selective inhibitor of FLT3 receptor tyrosine kinase (FLT3/ITD mutation). HP1142 is a benzoimidazole scaffold-based compound. HP1142 has the potential for the research of FLT3/ITD leukemia .
    HP1142
  • HY-145690
    HP1328

    		FLT3 Cancer
    HP1328 is a potent inhibitor of FLT3 receptor tyrosine kinase (FLT3/ITD mutation). HP1328 is a benzoimidazole scaffold-based compound. HP1328 significantly reduces the leukemia burden and prolongs the survival of mice with FLT3/ITD leukemia .
    HP1328
  • HY-111545
    BSc5371

    		FLT3 Cancer
    BSc5371 is a potent and irreversible FLT3 inhibitor, with Kds of 1.3, 0.83, 1.5, 5.8 and 2.3 nM for mutant FLT3(D835H), FLT3(ITD, D835V), FLT3(ITD, F691L), FLT3-ITD and wild type FLT3wt, respectively. BSc5371 is cytotoxic to FLT3-dependent cell lines .
    BSc5371
  • HY-162037
    CDDD11-8

    		CDK FLT3 Cancer
    CDDD11-8 is an orally active, potent and selective inhibitor of CDK9 and FLT3-ITD, with Ki values of 8 and 13 nM, respectively. CDDD11-8 reduces the proliferation of leukemia cell lines and was particularly effective against those harboring FLT3-ITD mutation .
    CDDD11-8
  • HY-139996
    Pomalidomide-C5-Dovitinib

    		PROTACs Apoptosis FLT3 c-Kit FGFR VEGFR PDGFR c-Fms Cancer
    Pomalidomide-C5-Dovitinib (compound 2) is a PROTAC containing Pomalidomide, Dovitinib and connected with CRBN. Pomalidomide-C5-Dovitinib shows enhanced antiproliferative effects against FLT3-ITD+ AML cells. Pomalidomide-C5-Dovitinib induces the degradation of the FLT3-ITD and KIT proteins in a ubiquitin-proteasome-dependent manner and completely blocks their downstream signaling pathway. Pomalidomide-C5-Dovitinib has the potential for the research of FLT3-ITD + acute myeloid leukemia .
    Pomalidomide-C5-Dovitinib
  • HY-128572
    FLT3-IN-6

    		FLT3 Cancer
    FLT3-IN-6 is a potent and selective inhibitor of FLT3-ITD (FLT3 mutation) with an IC50 of 1.336 nM .
    FLT3-IN-6
  • HY-158325
    PROTAC FLT-3 degrader 4

    		PROTACs FLT3 Apoptosis Cancer
    PROTAC FLT-3 degrader 4 is an orally active CRBN-based FLT3-PROTAC degrader that potently induces FLT3-ITD degradation through the ubiquitin-proteasome system. PROTAC FLT-3 degrader 4 shows highly selective to FLT3-ITD mutant acute myeloid leukemia (AML) cells. (Blue: CRBN ligand, Black: linker; Pink: FLT3 inhibitor) .
    PROTAC FLT-3 degrader 4
  • HY-153886
    Wu-5

    		FLT3 AMPK Apoptosis Cancer
    Wu-5 is a USP10 inhibitor that can inhibit FLT3 and AMPK pathways, induce FLT3-ITD degradation and induce apoptosis .
    Wu-5
  • HY-153857
    PHI-101

    		FLT3 Cancer
    PHI-101 is an orally active FLT3 inhibitor that overcomes resistance to multiple drug-resistant mutations. PHI-101 potently inhibits FLT3 single activating mutations (ITD or TKD mutants) and has inhibitory activity against FLT3 double (ITD/D835Y or ITD/F691L) and triple (ITD/D835Y/F691L) resistance mutations. PHI-101 has potential for research in relapsed or refractory acute myeloid leukemia (AML) .
    PHI-101
  • HY-120758
    SEL24-B489

    		Pim FLT3 Apoptosis Cancer
    SEL24-B489 is a potent, type I, orally active, dual PIM and FLT3-ITD inhibitor, with Kd values of 2 nM for PIM1, 2 nM for PIM2 and 3 nM for PIM3, respectively .
    SEL24-B489
  • HY-143286
    PF15

    		PROTACs FLT3 Cancer
    PF15 is a PROTAC connected by ligands for FLT3 kinase and CRBN. PF15 is a high selective FLT3-ITD degrader, with a DC50 of 76.7 nM. PF15 significantly inhibits the proliferation of FLT3-ITD-positive cells, can down-regulate the phosphorylation of FLT3 and STAT5. PF15 also inhibits tumor growth in mouse models and can be used in study of leukemia .
    PF15
  • HY-144782
    HDAC10-IN-2

    		HDAC Autophagy Cancer
    HDAC10-IN-2 (compound 10c) is a potent and highly selective HDAC10 inhibitor, with an IC50 of 20 nM. HDAC10-IN-2 modulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells .
    HDAC10-IN-2
  • HY-144779
    HDAC10-IN-1

    		HDAC Autophagy Cancer
    HDAC10-IN-1 (compound 13b) is a potent and highly selective HDAC10 inhibitor, with an IC50 of 58 nM. HDAC10-IN-1 modulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells .
    HDAC10-IN-1
  • HY-144782A
    HDAC10-IN-2 hydrochloride

    		HDAC Autophagy Cancer
    HDAC10-IN-2 hydrochloride (compound 10c) is a potent and highly selective HDAC10 inhibitor, with an IC50 of 20 nM. HDAC10-IN-2 hydrochloride modulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells .
    HDAC10-IN-2 hydrochloride
  • HY-155770
    FLT3-IN-20

    		FLT3 Cancer
    FLT3-IN-20 (compound 34f) is a potent FLT3 inhibitor with IC50 values of 1 and 4 nM for FLT3-D835Y and FLT3-ITD, respectively. FLT3-IN-20 has anti-proliferation efficacy in FLT3-ITD-positive AML cell lines MV4-11 and MOLM-13 (7 and 9 nM, respectively) and the MOLM-13 variant (4 nM) with the FLT3-ITD-D835Y mutation. FLT3-IN-20 can be used in research of cancer .
    FLT3-IN-20
  • HY-143286A
    PF15 TFA

    		PROTACs FLT3 Cancer
    PF15 TFA is a PROTAC connected by ligands for FLT3 kinase and CRBN. PF15 TFA is a high selective FLT3-ITD degrader，with a DC50 of 76.7 nM. PF15 TFA significantly inhibits the proliferation of FLT3-ITD-positive cells，can down-regulate the phosphorylation of FLT3 and STAT5. PF15 TFA also inhibits tumor growth in mouse models and can be used in study of leukemia .
    PF15 TFA
  • HY-168213
    FLT3-IN-27

    		FLT3 Cancer
    FLT3-IN-27 (compound 49) is a FLT3-ITD inhibitor with the IC50 of 174 nM. FLT3-IN-27 inhibits cell growth and increases the number of cells in the G1 phase of the cell cycle and can be used for study of acute myeloid leukemia .
    FLT3-IN-27
  • HY-18161
    CCT241736

    		FLT3 Aurora Kinase Cancer
    CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor, which inhibits Aurora kinases (Aurora-A Kd, 7.5 nM, IC50, 38 nM; Aurora-B Kd, 48 nM), FLT3 kinase (Kd, 6.2 nM), and FLT3 mutants including FLT3-ITD (Kd, 38 nM) and FLT3(D835Y) (Kd, 14 nM).
    CCT241736
  • HY-116129
    BPR1J-340

    		FLT3 Apoptosis Cancer
    BPR1J-340 is a potent FLT3 inhibitor with an IC50 of ~25 nM. BPR1J-340 inhibits the phosphorylation of FLT3 and STAT5 and triggered apoptosis in FLT3-ITD + acute myeloid leukemia (AML) cells. BPR1J-340 exhibits significant anti-tumor activities .
    BPR1J-340
  • HY-162032
    FLT3-IN-25

    		FLT3 Cancer
    FLT3-IN-25 (compound 17) is a potent inhibitor of FLT3, with IC50s of 1.2 nM, 1.4 nM and 1.1 nM for FLT3-WT, FLT3-D835Y and FLT3-ITD, respectively. FLT3-IN-25 plays an important role in acute myeloid leukemia (AML) .
    FLT3-IN-25
  • HY-155594
    LT-540-717

    		FLT3 Cancer
    LT-540-717 (compound 32) is a potent FLT3 inhibitor (IC50=0.62 nM) with antiproliferative activity. LT-540-717 also inhibits several acquired FLT3 mutations, FLT3 (ITD, D835V), FLT3 (ITD, F691L), FLT3 (D835Y) and FLT3 (D835V). LT-540-717 has potential to be an anti-AML agent .
    LT-540-717
  • HY-N10221
    Petromurin C

    		Apoptosis Cancer
    Petromurin C is a bisindolylbenzenoid compound isolated from the ascostromata of Petromycesmuricatus. Petromurin C induces protective autophagy and apoptosis in FLT3-ITD-positive AML .
    Petromurin C
  • HY-13001
    Quizartinib
    Maximum Cited Publications
    32 Publications Verification

    AC220; AC708

    		 FLT3 Ligands for Target Protein for PROTAC Apoptosis Cancer
    Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis .
    Quizartinib
  • HY-144777
    FLT3-IN-14

    		FLT3 Apoptosis Cancer
    FLT3-IN-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model .
    FLT3-IN-14
  • HY-148521
    PROTAC FLT3/CDK9 degrader-1

    		CDK FLT3 PROTACs Apoptosis Cancer
    PROTAC FLT3/CDK9 degrader-1 is a potent FLT3 and CDK9 dual PROTAC degrader. PROTAC FLT3/CDK9 degrader-1 induces apoptosis and effective degradation of target proteins FLT3 and CDK9. PROTAC FLT3/CDK9 degrader-1 has the potential for the research of FLT3-ITD mutated AML .
    PROTAC FLT3/CDK9 degrader-1
  • HY-162936
    SILA-123

    		FLT3 Apoptosis Cancer
    SILA-123 is a FLT3 inhibitor (FLT3-WT: IC50=2.1 nM; FLT3-ITD: IC50=1.0 nM). SILA-123 inhibits FLT3 phosphorylation and downstream signaling pathways, leading to apoptosis by arresting cell cycle progression at the G0/G1 phase. SILA-123 can be used in the study of acute myeloid leukemia .
    SILA-123
  • HY-13001R
    Quizartinib (Standard)

    		FLT3 Ligands for Target Protein for PROTAC Apoptosis Autophagy Cancer
    Quizartinib (Standard) is the analytical standard of Quizartinib. This product is intended for research and analytical applications. Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis .
    Quizartinib (Standard)
  • HY-14217
    Quizartinib dihydrochloride
    Maximum Cited Publications
    32 Publications Verification

    AC220 dihydrochloride

    		 FLT3 Apoptosis Ligands for Target Protein for PROTAC Cancer
    Quizartinib dihydrochloride (AC220 dihydrochloride) is the dihydrochloride salt form of Quizartinib (HY-13001). Quizartinib dihydrochloride is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib dihydrochloride inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib dihydrochloride can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib dihydrochloride induces apoptosis .
    Quizartinib dihydrochloride
  • HY-110026
    GTP-14564

    		FLT3 Cancer
    GTP-14564 is a tyrosine kinase inhibitor targeting to internal tandem duplication (ITD) and FLT3. GTP-14564 inhibits FLT3 ligand-dependent growth in Ba/F3 leukemia cells .
    GTP-14564
  • HY-146749
    FLT3/TrKA-IN-1

    		FLT3 Trk Receptor Apoptosis Cancer
    FLT3/TrKA-IN-1 is a potent FLT3/TrKA dual kinase inhibitor with the IC50s of 43.8 nM, 97.2 nM, 92.5 nM and 23.6 nM for FLT3, FLT3-ITD, FLT3-TKD and TrKA, respectively. FLT3/TrKA-IN-1 induces cell cycle arrest at the G0/G1 phase as well as apoptosis and shows antiproliferative activity in vitro. FLT3/TrKA-IN-1 has the potential for the research of Acute myeloid leukemia (AML) .
    FLT3/TrKA-IN-1
  • HY-156410
    FLT3-IN-23

    		FLT3 Cancer
    FLT3-IN-23 (compound 15) is an inhibitor of JFMS-like tyrosine kinase 3 (FLT3) with an IC50 of 7.42 nM. FLT3-IN-23 has antiproliferative activities against BaF3 cells carrying various FLT3-TKD and FLT3-ITD-TKD mutations .
    FLT3-IN-23
  • HY-111249
    TTT 3002

    		FLT3 Cancer
    TTT 3002 is a potent and orally active FLT3 inhibitor. TTT 3002 potently inhibits FLT3 phosphorylation by activating mutations at residue D835, with an IC50 of 0.2 nM. TTT 3002 can be used for AML (acute myeloid leukemia) research .
    TTT 3002
  • HY-126920
    AFG206

    		FLT3 Apoptosis Cardiovascular Disease
    AFG206 is a first-generation ATP competitive “type II” FLT3 inhibitor. AFG206 potently inhibits cell proliferation (IC50 around 0.1 µM) via induction of Apoptosis in FLT3-ITD-Ba/F3 cells and D835Y-Ba/F3 cells. AFG206 is promising for research of acute myeloid leukemia .
    AFG206
  • HY-131230
    Desmorpholinyl Quizartinib-PEG2-COOH

    		Target Protein Ligand-Linker Conjugates Cancer
    Desmorpholinyl Quizartinib-PEG2-COOH incorporates a ligand for FLT-3, and a PEG-based PROTAC linker. Desmorpholinyl Quizartinib-PEG2-COOH can be used in the synthesis of PROTAC FLT-3 degrader 1 (HY-114323). PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM .
    Desmorpholinyl Quizartinib-PEG2-COOH
  • HY-100368
    MELK-8a
    3 Publications Verification

    NVS-MELK8a

    		 MELK PDGFR Haspin Kinase Cancer
    MELK-8a (NVS-MELK8a) is a highly potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor with IC50 of 2 nM. MELK-8a also inhibits Flt3 (ITD), Haspin, PDGFRα with IC50s of 0.18, 0.19, and 0.42 μM, respectively. MELK plays an essential role in regulating cell mitosis in a subset of cancer cells .
    MELK-8a
  • HY-114323
    PROTAC FLT-3 degrader 1

    		PROTACs FLT3 Apoptosis STAT MEK ERK Cancer
    PROTAC FLT-3 degrader 1 is an effective and selective FLT-3 PROTAC degrader with an IC50 of 0.6 nM. PROTAC FLT-3 degrader 1 inhibits both FLT-3 and FLT-3 ITD mutants. PROTAC FLT-3 degrader 1 has the activity of anti-proliferation and induction of apoptosis, which can be used in the study of tumor. (Pink: FLT3 ligand (HY-168702); Black: Linker (HY-124380); Blue: VHL ligand (HY-125845)) .
    PROTAC FLT-3 degrader 1
  • HY-124500
    AC-4-130
    4 Publications Verification

    		 STAT Apoptosis Cancer
    AC-4-130 is a potent STAT5 SH2 domain inhibitor. AC-4-130 directly binds to STAT5 and disrupts STAT5 activation, dimerization, nuclear translocation, and STAT5-dependent gene transcription. AC-4-130 induces cell cycle arrest and apoptosis in FLT3-ITD-driven leukemic cells. AC-4-130 has anti-cancer activity and can efficiently block pathological levels of STAT5 activity in acute myeloid leukemia (AML) .
    AC-4-130

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